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Lonodelestat TFA

(Synonyms: POL6014 TFA) 目录号 : GC69394

Lonodelestat TFA (POL6014 TFA) 是有效的、具有口服活性的、选择性的人中性粒细胞弹性蛋白酶(hNE) 的肽类抑制剂。Lonodelestat TFA 具有囊性纤维化 (CF) 研究的潜力 .

Lonodelestat TFA Chemical Structure

规格 价格 库存 购买数量
10mg
¥4,050.00
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25mg
¥8,550.00
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50mg
¥13,680.00
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100mg
¥21,960.00
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Sample solution is provided at 25 µL, 10mM.

Description

Lonodelestat TFA (POL6014 TFA) is a potent, orally active and selective peptide inhibitor of human neutrophil elastase (hNE). Lonodelestat TFA has the potential for the research of cystic fibrosis (CF)[1][2][3].

Lonodelestat (POL6014) significantly and efficiently reduced the inflammatory processes of ALI in HNE treated mice[1].
Lonodelestat (POL6014, 0.1, 0.5, 2 and 10 mg/kg, intranasally administered) dose-dependently and significantly reduces the number of macrophages, epithelial cells, neutrophils and lymphocytes recovered in BAL. The maximum inhibition was reached at 2 mg/kg in reducing neutrophils by 65% (p<0.001), epithelial cells by 68% (p<0.001), macrophages by 33% (p<0.001) and lymphocytes by 77% (p<0.001)[1].

[1]. Lagente V, et al. A novel Protein Epitope Mimetic (PEM) neutrophil elastase (NE) inhibitor, POL6014, inhibits human NE-induced acute lung injury in mice. ATS, San Diego, May 15-20, 2009.
[2]. Odile Sellier-Kessler, et al. Inhibition of lung inflammation by a protein epitope mimetic (PEM) neutrophil elastase inhibitor, POL6014, in a sub-chronic tobacco smoke (TS) model in mice. European Respiratory Journal 2013 42: 1762.
[3]. Barth P, et al. Single dose escalation studies with inhaled POL6014, a potent novel selective reversible inhibitor of human neutrophil elastase, in healt volunteers and subjects with cystic fibrosis. J Cyst Fibros. 2020 Mar;19(2):299-304.

化学性质

Cas No. SDF Download SDF
别名 POL6014 TFA
分子式 C73H112F3N15O21 分子量 1592.75
溶解度 H2O : 50 mg/mL (31.39 mM; Need ultrasonic) 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 0.6278 mL 3.1392 mL 6.2784 mL
5 mM 0.1256 mL 0.6278 mL 1.2557 mL
10 mM 0.0628 mL 0.3139 mL 0.6278 mL
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